Assay Detail
Binding
CHEMBL3108481
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Antagonist activity at rat P2X4 receptor assessed as inhibition of ATP-induced calcium influx preincubated for 30 mins followed by ATP addition by Fluo-4 AM dye-based fluorescence assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Carbamazepine derivatives with P2X4 receptor-blocking activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 4.25 | 4.45 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3103375 | — | — | 1 | 4.45 |
| CHEMBL1483754 | — | — | 1 | 4.37 |
| CHEMBL3103385 | — | — | 1 | 4.26 |
| CHEMBL3103372 | — | — | 1 | 4.16 |
| CHEMBL3103371 | — | — | 1 | 4.02 |
| CHEMBL3103369 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3103375 | — | IC50 | = | 35900.0 | nM | 4.45 |
| CHEMBL1483754 | — | IC50 | = | 43000.0 | nM | 4.37 |
| CHEMBL3103385 | — | IC50 | = | 54600.0 | nM | 4.26 |
| CHEMBL3103372 | — | IC50 | = | 69300.0 | nM | 4.16 |
| CHEMBL3103371 | — | IC50 | = | 95800.0 | nM | 4.02 |
| CHEMBL3103369 | — | IC50 | = | 109000.0 | nM | - |